TG 100801

• CAT Number: I005219
• CAS Number: 867331-82-6
• Molecular Formula: C33H30ClN5O3
• Molecular Weight: 580.08
• Purity: ≥95%
• Synonyms: [4-chloro-3-[5-methyl-3-[4-(2-pyrrolidin-1-ylethoxy)anilino]-1,2,4-benzotriazin-7-yl]phenyl] benzoate
• Target: VEGFR
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• InChI: 1S/C33H30ClN5O3/c1-22-19-24(28-21-27(13-14-29(28)34)42-32(40)23-7-3-2-4-8-23)20-30-31(22)36-33(38-37-30)35-25-9-11-26(12-10-25)41-18-17-39-15-5-6-16-39/h2-4,7-14,19-21H,5-6,15-18H2,1H3,(H,35,36,38)
• InChIKey: JMGXJHWTVBGOKG-UHFFFAOYSA-N
• SMILES: CC1=CC(=CC2=C1N=C(N=N2)NC3=CC=C(C=C3)OCCN4CCCC4)C5=C(C=CC(=C5)OC(=O)C6=CC=CC=C6)Cl

TG 100801 (Cat No.: I005219) is a small-molecule inhibitor targeting vascular endothelial growth factor receptor-2 (VEGFR-2) and platelet-derived growth factor receptor (PDGFR), developed for the treatment of ocular diseases such as age-related macular degeneration (AMD) and diabetic macular edema. Designed for topical ocular delivery, TG 100801 aims to reduce abnormal blood vessel growth and vascular leakage in the retina. By blocking angiogenic signaling pathways, it offers a non-invasive alternative to intravitreal injections. TG 100801 is primarily used in preclinical and clinical research for retinal disorders.

Reference

[1]. Mousa, Shaker A.; Mousa, Shaymaa S. Current status of vascular endothelial growth factor inhibition in age-related macular degeneration. BioDrugs (2010), 24(3), 183-194.
[2]. Doukas, John; Mahesh, Sankaranarayana; Umeda, Naoyasu et al. Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema. Journal of Cellular Physiology (2008), 216(1), 29-37.
[3]. A Phase 1 Safety Study of TG100801 Eye Drops in Healthy Volunteers.
[4]. Palanki MS, Akiyama H, Campochiaro P et al. Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration. J Med Chem. 2008 Mar 27;51(6):1546-59.
[5]. Chappelow AV, Kaiser PK. Neovascular age-related macular degeneration: potential therapies. Drugs. 2008;68(8):1029-36.